中药化学生物学（traditional Chinese medicine chemical biology，TCMCB）是中医药现代化进程中催生的一门交叉性学科，以中医药理论为指导，中药活性成分为分子探针，聚焦中药活性成分作用靶点的精准鉴定、信号通路调控及生命过程干预机制，为中医药科学内涵的现代化阐释及国际化推广搭建了关键技术支撑。系统梳理了TCMCB的学科定位、核心技术与方法，总结了其在中药活性成分作用机制解析、创新药物研发等领域的应用及面临的瓶颈，并重点整合近10年原创性研究成果。TCMCB已逐步构建起“活性成分筛选-靶点精准鉴定-作用机制解析-临床转化应用”的完整研究体系，推动中医药理论从经验描述向机制驱动转变，为现代医学疾病治疗及创新药物研发提供了新策略。未来需着力突破中药活性成分供给、靶点精准验证、国际化评价体系等关键问题，构建自主知识产权技术平台和全球传统药物靶点数据库，助力中医药向现代精准医学发展。

Traditional Chinese medicine chemical biology (TCMCB) is an interdisciplinary discipline emerging in the modernization of traditional Chinese medicine (TCM). Guided by TCM theories, TCMCB employs bioactive components from Chinese medicines as molecular probes, focusing on the precise identification of action targets, regulation of signaling pathways, and intervention mechanisms of life processes induced by TCM bioactive ingredients. It provides critical technical support for the modern interpretation of the scientific connotation of TCM and its international promotion. This paper systematically reviews the disciplinary orientation, core technologies and methodologies of TCMCB, summarizes its applications and bottlenecks in the mechanistic elucidation of TCM bioactive components and innovative drug discovery and development, and highlights original research achievements over the past decade. TCMCB has gradually established an integrated research paradigm: “bioactive component screening-precise target identification-mechanism elucidation-clinical translational application” promoting the transformation of TCM theories from empirical description to mechanism-driven interpretation, and offering novel strategies for disease treatment in modern medicine and innovative drug development. Future efforts should focus on overcoming key challenges including the supply of TCM bioactive components, precise validation of targets, and international evaluation systems. Meanwhile, the construction of technology platforms with independent intellectual property rights and a global target database for traditional medicines will facilitate the advancement of TCM toward modern precision medicine.

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江西省自然科学基金青年项目（20252BAC200578）；江西省职业早期青年人才培养项目（20252BEJ730276）；赣州市科技计划项目（2025XDCE0014，2025XDCE0032）